Home Cytoskeletal Signaling ADC Cytotoxin inhibitor MMAE (Monomethyl auristatin E)

연구용

MMAE (Monomethyl auristatin E) Antineoplastic Agent

제품 번호: S7721

MMAE (Monomethyl auristatin E) is a synthetic antineoplastic agent. It is also a microtubule-disrupting agent .
MMAE (Monomethyl auristatin E) ADC Cytotoxin inhibitor Chemical Structure

화학 구조

분자량: 717.98

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품질 관리 (Quality Control)

배치: 순도: 99.99%
99.99

세포 배양, 처리 및 작업 농도
(Cell Culture, Treatment & Working Concentration)

세포주 분석 유형 농도 배양 시간 제형 활성 설명 PMID
KB Antiproliferative assay 4 days Antiproliferative activity against human KB cells after 4 days by XTT assay, IC50=0.00019μM 23845743
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 23845743
A549 Antiproliferative assay 4 days Antiproliferative activity against human A549 cells after 4 days by XTT assay, IC50=0.00059μM 23845743
non-small cell lung cancer cells Cytotoxicity assay 0.5 to 1 nM 4 days Cytotoxicity against human non-small cell lung cancer cells at 0.5 to 1 nM after 4 days by XTT assay 23845743
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 25431858
MDA-MB-361 Cytotoxicity assay Cytotoxicity against human MDA-MB-361 cells assessed as cell viability incubated fore 4 days by MTS assay, GI50=0.00049μM 25431858
NCI-N87 Cytotoxicity assay Cytotoxicity against human NCI-N87 cells assessed as cell viability incubated fore 4 days by MTS assay, GI50=0.00054μM 25431858
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 28211277
DU145 Growth inhibition assay 48 hrs Growth inhibition of human DU145 cells incubated for 48 hrs by MTT assay, GI50=0.000418μM 28211277
SF268 Growth inhibition assay 48 hrs Growth inhibition of human SF268 cells incubated for 48 hrs by MTT assay, GI50=0.000432μM 28211277
KM20L2 Growth inhibition assay 48 hrs Growth inhibition of human KM20L2 cells incubated for 48 hrs by MTT assay, GI50=0.000599μM 28211277
NCI-H460 Growth inhibition assay 48 hrs Growth inhibition of human NCI-H460 cells incubated for 48 hrs by MTT assay, GI50=0.000683μM 28211277
HCT116 Function assay 0.5 mM 24 hrs Effect on mitochondrial respiration in human HCT116 cells expressing carbonic anhydrase 9 assessed as reduction in oxygen consumption rate at 0.5 mM after 24 hrs under hypoxic condition by Western blot analysis 28895394
DU145 Growth inhibition assay 48 hrs Growth inhibition of human DU145 cells after 48 hrs by SRB assay, GI50=0.000418μM 28895394
SF268 Growth inhibition assay 48 hrs Growth inhibition of human SF268 cells after 48 hrs by SRB assay, GI50=0.000432μM 28895394
KM20L2 Growth inhibition assay 48 hrs Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay, GI50=0.000599μM 28895394
NCI-H460 Growth inhibition assay 48 hrs Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay, GI50=0.000683μM 28895394
MCF7 Growth inhibition assay 48 hrs Growth inhibition of human MCF7 cells after 48 hrs by SRB assay, GI50=0.000404μM 28926240
DU145 Growth inhibition assay 48 hrs Growth inhibition of human DU145 cells after 48 hrs by SRB assay, GI50=0.000418μM 28926240
SF268 Growth inhibition assay 48 hrs Growth inhibition of human SF268 cells after 48 hrs by SRB assay, GI50=0.000432μM 28926240
KM20L2 Growth inhibition assay 48 hrs Growth inhibition of human KM20L2 cells after 48 hrs by SRB assay, GI50=0.000599μM 28926240
NCI-H460 Growth inhibition assay 48 hrs Growth inhibition of human NCI-H460 cells after 48 hrs by SRB assay, GI50=0.000683μM 28926240
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 28972755
A549 Antiproliferative assay 72 hrs Antiproliferative activity against human A549 cells after 72 hrs by MTS assay, EC50=0.0005μM 28972755
SKOV3 Cytotoxicity assay 2 days Cytotoxicity against human SKOV3 cells after 2 days by cell titer 96 aqueous one solution based assay, IC50=0.00066μM 29454703
A549 Cytotoxicity assay 2 days Cytotoxicity against human A549 cells after 2 days by cell titer 96 aqueous one solution based assay, IC50=0.0013μM 29454703
L1210 Cytotoxicity assay 2 days Cytotoxicity against mouse L1210 cells after 2 days by cell titer 96 aqueous one solution based assay, IC50=0.0021μM 29454703
NCI-H524 Cytotoxicity assay 2 hrs Cytotoxicity in human NCI-H524 cells pre-incubated for 2 hrs followed by compound wash out and subsequently incubated for 70 hrs by Cell Titer Glo assay, IC50=0.0037μM 30735385
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화학 정보, 보관 및 안정성 (Chemical Information, Storage & Stability)

분자량 717.98 화학식
C39H67N5O7
 
 보관 (수령일로부터)
CAS 번호 474645-27-7 SDF 다운로드 원액 보관

동의어 SGD-1010 Smiles CCC(C)C(C(CC(=O)N1CCCC1C(C(C)C(=O)NC(C)C(C2=CC=CC=C2)O)OC)OC)N(C)C(=O)C(C(C)C)NC(=O)C(C(C)C)NC

용해도 (Solubility)

In vitro
배치:

DMSO : 100 mg/mL (139.27 mM)
(수분으로 오염된 DMSO는 용해도를 감소시킬 수 있습니다. 신선하고 무수 DMSO를 사용하십시오.)

Ethanol : 100 mg/mL

Water : Insoluble

몰농도 계산기

질량 농도 부피 분자량
희석 계산기 분자량 계산기

In vivo
배치:

생체 내 제형 계산기 (투명한 용액)

1단계: 아래 정보 입력 (권장: 실험 중 손실을 고려하여 추가 동물 포함)

mg/kg g μL

2단계: 생체 내 제형 입력 (이것은 계산기일 뿐 제형이 아닙니다. 용해도 섹션에 생체 내 제형이 없는 경우 먼저 당사에 문의하십시오.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

계산 결과:

작업 농도: mg/ml;

DMSO 원액 준비 방법: mg 약물 사전 용해 μL DMSO ( 원액 농도 mg/mL, 농도가 해당 약물 배치의 DMSO 용해도를 초과하는 경우 먼저 당사에 문의하십시오. )

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가μL PEG300, 혼합하고 투명하게 한 다음 추가μL Tween 80, 혼합하고 투명하게 한 다음 추가 μL ddH2O, 혼합하고 투명하게 합니다.

생체 내 제형 준비 방법: 취하다 μL DMSO 원액, 다음 추가 μL 옥수수 기름, 혼합하고 투명하게 합니다.

참고: 1. 다음 용매를 추가하기 전에 액체가 투명한지 확인하십시오.
2. 용매를 순서대로 추가해야 합니다. 다음 용매를 추가하기 전에 이전 추가에서 얻은 용액이 투명한 용액인지 확인해야 합니다. 와동, 초음파 또는 뜨거운 물 중탕과 같은 물리적 방법을 사용하여 용해를 도울 수 있습니다.

작용 메커니즘 (Mechanism of Action)

시험관 내(In vitro)

When coupled to cAC10, MMAE shows selective cytotoxicity in CD30+ cells, and induces G2/M-phase growth arrest and cell death through the induction of apoptosis.

When coupled to anti-CD79b antibody, anti–CD79b-vcMMAE has very potent and broad activity across a large panel of NHL cell lines in vitro.

When coupled to anti-HER2 antibody, hertuzumab-vc-MMAE can also be effectively internalized and potently kill HER2 over-expressing tumor cells.

생체 내(In vivo)

In the Karpas 299 ALCL model, cAC10-vcMMAE (1 mg/kg, i.v.) induces complete, durable tumor regression, while free MMAE (0.36 mg/kg) doesn’t produce detectable antitumor activity.

In mouse xenograft models of NHL, anti–CD79b-vcMMAE (7 mg/kg, p.o.) strikingly results in sustained complete tumor remission.

참조
  • [4] https://pubmed.ncbi.nlm.nih.gov/28923397/

임상시험 정보 (Clinical Trial Information)

(데이터 출처 https://clinicaltrials.gov, 업데이트 날짜 2024-05-22)

NCT 번호 모집 조건 스폰서/협력자 시작일 단계
NCT06395103 Not yet recruiting
B-cell Acute Lymphoblastic Leukemia|Diffuse Large B-cell Lymphoma|Burkitt Lymphoma|Neuroblastoma|Ewing Sarcoma
Merck Sharp & Dohme LLC
 June 4 2024 Phase 1|Phase 2
NCT06227156 Recruiting
Castration-resistant Prostate Cancer
RemeGen Co. Ltd.
 April 8 2024 Phase 1
NCT06265727 Recruiting
Solid Tumor Adult
Corbus Pharmaceuticals Inc.|CSPC Zhongnuo Pharmaceutical (Shijiazhuang) Co. Ltd.
 April 1 2024 Phase 1|Phase 2
NCT06351020 Not yet recruiting
Locally Advanced or Metastatic GC and GCJ Adenocarcinoma
LaNova Medicines Zhejiang Co. Ltd.|LaNova Medicines Limited
 April 1 2024 Phase 3